Catalog Number: 3140
Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Biological Activity
Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM) and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2) (IC50 = 171 nM).
Technical Data
  • M.Wt:
    249.7
  • Formula:
    C12H11N3O.HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    942425-68-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
    Anderson et al.
    J.Med.Chem., 2007;50:2647
  2. Stopping replication, at the beginning.
    Jackson
    Nature Chem.Biol., 2008;4:331
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:

2 Citations: Showing 1 - 2
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  1. A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response.
    Authors: FitzGerald Et al.
    PLoS One 2014;9:e98891
  2. Geminin overexpression prevents the completion of topoisomerase IIα chromosome decatenation, leading to aneuploidy in human mammary epithelial cells.
    Authors: Gardner Et al.
    Breast Cancer Res 2011;13:R53

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